TWI527809B - 作為ｃｒｔｈ２拮抗劑之吡唑化合物 - Google Patents

Info

Publication number

TWI527809B

TWI527809B TW101102302A TW101102302A TWI527809B TW I527809 B TWI527809 B TW I527809B TW 101102302 A TW101102302 A TW 101102302A TW 101102302 A TW101102302 A TW 101102302A TW I527809 B TWI527809 B TW I527809B

Authority

TW

Taiwan

Prior art keywords

pharmaceutically acceptable

acceptable salt

formula

pyrazole compound

group

Prior art date

2011-01-24

Links

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• 239000005557 antagonist Substances 0.000 title claims description 30
• 150000003217 pyrazoles Chemical class 0.000 title claims description 14
• 150000001875 compounds Chemical class 0.000 claims description 121
• -1 pyrazole compound Chemical class 0.000 claims description 113
• 150000003839 salts Chemical class 0.000 claims description 73
• 108050000258 Prostaglandin D receptors Proteins 0.000 claims description 50
• QTBSBXVTEAMEQO-UHFFFAOYSA-N Acetic acid Chemical compound CC(O)=O QTBSBXVTEAMEQO-UHFFFAOYSA-N 0.000 claims description 45
• 125000004432 carbon atom Chemical group C* 0.000 claims description 31
• 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 29
• 229910052799 carbon Inorganic materials 0.000 claims description 21
• 125000005843 halogen group Chemical group 0.000 claims description 21
• 229910052739 hydrogen Inorganic materials 0.000 claims description 20
• 239000003112 inhibitor Substances 0.000 claims description 19
• 239000003795 chemical substances by application Substances 0.000 claims description 18
• 201000010099 disease Diseases 0.000 claims description 18
• 229910052757 nitrogen Inorganic materials 0.000 claims description 17
• 239000008194 pharmaceutical composition Substances 0.000 claims description 17
• 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims description 15
• 230000000694 effects Effects 0.000 claims description 15
• 125000000217 alkyl group Chemical group 0.000 claims description 13
• 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 13
• 229910052760 oxygen Inorganic materials 0.000 claims description 13
• 229910052717 sulfur Inorganic materials 0.000 claims description 12
• 208000035475 disorder Diseases 0.000 claims description 11
• 150000001412 amines Chemical class 0.000 claims description 10
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• 239000001257 hydrogen Substances 0.000 claims description 10
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• 238000002360 preparation method Methods 0.000 claims description 10
• 239000000126 substance Substances 0.000 claims description 10
• 125000005842 heteroatom Chemical group 0.000 claims description 9
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• 229940123932 Phosphodiesterase 4 inhibitor Drugs 0.000 claims description 8
• 208000027866 inflammatory disease Diseases 0.000 claims description 8
• YEESKJGWJFYOOK-IJHYULJSSA-N leukotriene D4 Chemical compound CCCCC\C=C/C\C=C/C=C/C=C/[C@H]([C@@H](O)CCCC(O)=O)SC[C@H](N)C(=O)NCC(O)=O YEESKJGWJFYOOK-IJHYULJSSA-N 0.000 claims description 8
• 239000002587 phosphodiesterase IV inhibitor Substances 0.000 claims description 8
• 239000003246 corticosteroid Substances 0.000 claims description 7
• 208000015181 infectious disease Diseases 0.000 claims description 7
• 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 7
• 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 7
• 125000004191 (C1-C6) alkoxy group Chemical group 0.000 claims description 6
• 125000002373 5 membered heterocyclic group Chemical group 0.000 claims description 6
• 125000004070 6 membered heterocyclic group Chemical group 0.000 claims description 6
• 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims description 6
• 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims description 6
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• 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 5
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• 125000004093 cyano group Chemical group *C#N 0.000 claims description 4
• 125000000753 cycloalkyl group Chemical group 0.000 claims description 4
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• 101710149862 C-C chemokine receptor type 3 Proteins 0.000 claims description 3
• UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 3
• 150000002367 halogens Chemical class 0.000 claims description 3
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• 125000004438 haloalkoxy group Chemical group 0.000 claims description 2
• 229910052736 halogen Inorganic materials 0.000 claims description 2
• 125000001820 oxy group Chemical group [*:1]O[*:2] 0.000 claims description 2
• 125000000951 phenoxy group Chemical group [H]C1=C([H])C([H])=C(O*)C([H])=C1[H] 0.000 claims description 2
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• 150000002431 hydrogen Chemical class 0.000 claims 3
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• QXSIEYYKCAVRMN-UHFFFAOYSA-N 2-[1-[[4-[(3-ethyl-7-fluoro-1-benzofuran-2-carbonyl)amino]phenyl]methyl]-3,5-dimethylpyrazol-4-yl]acetic acid Chemical compound O1C2=C(F)C=CC=C2C(CC)=C1C(=O)NC(C=C1)=CC=C1CN1N=C(C)C(CC(O)=O)=C1C QXSIEYYKCAVRMN-UHFFFAOYSA-N 0.000 claims 1
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• JJXPTUWJVQUHKN-UHFFFAOYSA-N methoxy-5 benzofuranne Natural products COC1=CC=C2OC=CC2=C1 JJXPTUWJVQUHKN-UHFFFAOYSA-N 0.000 claims 1
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